INTRODUCTION TO PHARMACOLOGY PHARMACOLOGY Greek Pharmacon drug logos

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INTRODUCTION TO PHARMACOLOGY

INTRODUCTION TO PHARMACOLOGY

PHARMACOLOGY (Greek “Pharmacon” – drug, “logos” teaching) The science that studies the interaction of

PHARMACOLOGY (Greek “Pharmacon” – drug, “logos” teaching) The science that studies the interaction of the chemical substances with live organisms, drugs administration for treatment and prophylaxis of various diseases and pathological processes

• Pharmaceutical explosion • Nowadays there are over 350 thousand drugs in the

• Pharmaceutical explosion • Nowadays there are over 350 thousand drugs in the world which are used for different diseases • In Ukraine nearly 14 thousand drugs are registered now and allowed for administration as curative agents • The volume of world pharmaceutical market annually – 400 -600 billion $ • Till 2015 – 1, 1 trillion $

Ukraine: 128 preparations of Diclofenac-sodium, 60 – Paracetamol (Acetaminophen) For each drug - only

Ukraine: 128 preparations of Diclofenac-sodium, 60 – Paracetamol (Acetaminophen) For each drug - only single international name and different trade names

Nadolol – international name Corgard – trade name

Nadolol – international name Corgard – trade name

Paracetamol (Ukraine)

Paracetamol (Ukraine)

Milistan (Ukraine)

Milistan (Ukraine)

Farmacitron (Ukraine)

Farmacitron (Ukraine)

Becotide = Beclometh – trade name Beclomethasone dipropionate – international name

Becotide = Beclometh – trade name Beclomethasone dipropionate – international name

• Brand – original drug which is defended by patent and may be

• Brand – original drug which is defended by patent and may be produced during patent term only by this pharmaceutical firm (company) • Generic – when term of patent is discontinued the drug may be produced by different pharmaceutical companies under new product (trade) names but at the basis of original active substance (similar quantity, route of administration etc. ) • All generics are much more cheaper compared to brands, that is the main reason – why they are so popular among the patients

GENERICS • UK, Deutschland, French, Holland, Denmark – the part of generics among all

GENERICS • UK, Deutschland, French, Holland, Denmark – the part of generics among all drugs is 50 -75 % (in Ukraine – the majority of drugs) • Market volume of generics In Europe is over 10 billion $ annually

Brand generic – the same bioavailability speed and level of absorption of active substance

Brand generic – the same bioavailability speed and level of absorption of active substance after administration in equal doses under the same conditions

Bioavailability of drugs complex of pharmacokinetic processes that maintenances active concentration of drug in

Bioavailability of drugs complex of pharmacokinetic processes that maintenances active concentration of drug in the area of specific receptors (part of administered drug that reaches the systemic circulation and effects specific receptors)

Bioavailability – to study some pharmacokinetic parameters concentration Cmax AUC Area under curve Tmax

Bioavailability – to study some pharmacokinetic parameters concentration Cmax AUC Area under curve Tmax time

Side effects (SE) of drugs • Take 5 th place among causes of mortality

Side effects (SE) of drugs • Take 5 th place among causes of mortality in the whole world after cardiacvascular diseases, malignant tumors, lungs diseases, traumas • Among stationary patients frequency of SE after introduction of drugs makes 2 -40 %

focomelia Talidomide (katergan)

focomelia Talidomide (katergan)

PHARMACOKINETICS THE PART OF PHARMACOLOGY THAT CONCERNED WITH THE ABSORBTION, DISTRIBUTION, METABOLISM (BIOTRANSFORMATION) AND

PHARMACOKINETICS THE PART OF PHARMACOLOGY THAT CONCERNED WITH THE ABSORBTION, DISTRIBUTION, METABOLISM (BIOTRANSFORMATION) AND EXCRETION OF DRUGS WHAT THE ORGANISM DOES TO THE DRUGS

PHARMACODYNAMICS THE PART OF PHARMACOLOGY THAT CONCERNED WITH THE BIOCHEMICAL AND PHYSIOLOGICAL EFFECTS OF

PHARMACODYNAMICS THE PART OF PHARMACOLOGY THAT CONCERNED WITH THE BIOCHEMICAL AND PHYSIOLOGICAL EFFECTS OF DRUGS AND THEIR MODE OF ACTION IT INCLUDES THE DOSE-EFFECT RELATIONSHIP, FACTORS MODIFYING DRUG EFFECTS, DOSAGE, DRUG TOXICITY WHAT DRUGS DO TO THE ORGANISM

RECEPTOR THEORY OF DRUG ACTION • • Receptors – the places where drugs bind

RECEPTOR THEORY OF DRUG ACTION • • Receptors – the places where drugs bind to tissues: macromolecules, enzymes, channels, transport systems, genes Agonists: adrenalin, isadrine, morphine etc. Antagonists: atropin, anaprilin, dimedrol etc. Agonist-antagonist: labetolol ( 1, 1 -adreno-blocker, but activates 2 adrenoreceptors), pentazocin (agonist delta- and kappa-opiate receptors and mu-receptors antagonist)

Receptors – specific cell sites Opiate receptors steroid-receptor GABAc receptors Serotonine receptor

Receptors – specific cell sites Opiate receptors steroid-receptor GABAc receptors Serotonine receptor

Receptors - enzymes cholinesterase Cox - Cyclooxygenase MAO ACE - angiotensin converting enzyme

Receptors - enzymes cholinesterase Cox - Cyclooxygenase MAO ACE - angiotensin converting enzyme

Receptors – ionic channels sodium (Na+) channels Voltage-dependent potassium channels calcium channels

Receptors – ionic channels sodium (Na+) channels Voltage-dependent potassium channels calcium channels

thyroid hormone receptor - genes

thyroid hormone receptor - genes

PRESYSTEMIC ELIMINATION (first pass metabolism) presystemic elimination – extraction of the drug from blood

PRESYSTEMIC ELIMINATION (first pass metabolism) presystemic elimination – extraction of the drug from blood circulatory system during it’s first passage through the liver– it leads to decreasing of bioavailability (and therefore, decreasing of biological activity) of drugs propranolol (anaprilin), labetolol, aminazin, acetylsalicylic acid, labetolol, hydralasin, isadrin, cortizone, lidokain, morphin, pentazocin, organic nitrates, reserpin

PRESYSTEMIC ELIMINATION (first pass metabolism)

PRESYSTEMIC ELIMINATION (first pass metabolism)

• ONSET – the period between the moment of drug introduction to the

• ONSET – the period between the moment of drug introduction to the organism and the beginning of its action • DURATION OF DRUG ACTION – the period then specific effects of the drug are maintained • WIDENESS of therapeutic action (therapeutic window) – the distance between minimum therapeutic and minimum toxic doses of drug

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